2. Signaling Pathways
  3. Immunology/Inflammation
  4. Toll-like Receptor (TLR)

Toll-like Receptor (TLR)

Toll-like Receptor (TLR)

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Toll-like receptors (TLRs) are a class of proteins that play a key role in the innate immune system. They are single, membrane-spanning, non-catalytic receptors usually expressed in sentinel cells such as macrophages and dendritic cells, that recognize structurally conserved molecules derived from microbes. Once these microbes have breached physical barriers such as the skin or intestinal tract mucosa, they are recognized by TLRs, which activate immune cell responses. The TLRs include TLR1, TLR2, TLR3, TLR4, TLR5, TLR6, TLR7, TLR8, TLR9, TLR10, TLR11, TLR12, and TLR13. Toll-Like Receptors (TLRs) play a critical role in the early innate immune response to invading pathogens by sensing microorganism and are involved in sensing endogenous danger signals. TLRs are evolutionarily conserved receptors are homologues of the Drosophila Toll protein, discovered to be important for defense against microbial infection. TLRs recognize highly conserved structural motifs known as pathogen-associated microbial patterns (PAMPs), which are exclusively expressed by microbial pathogens.

Toll-like Receptor (TLR) Isoform Specific Products:

Toll-like Receptor (TLR) Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-146245
    ODN 1826
    		Agonist
    ODN 1826 (CpG 1826), a class B CpG ODN (oligodeoxynucleotide), is a TLR9 agonist. ODN 1826 promotes Apoptosis. ODN 1826 is an excellent immune stimulator with antitumor activity. ODN 1826 has protective effects on the heart. ODN 1826 sequence: 5’-tccatgacgttcctgacgtt-3’.
    ODN 1826
  • HY-123942
    Diprovocim
    		Agonist 98.82%
    Diprovocim is a potent TLR1/TLR2 agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC50=110 pM). Diprovocim stimulates the release of TNF-α from mouse macrophages (EC50=1.3 nM). Diprovocim activates downstream MAPK and NF-κB signaling pathway. Diprovocim displays strong adjuvant activity in mice, particularly abetting cellular immune responses.
    Diprovocim
  • HY-135748
    Polyinosinic-polycytidylic acid sodium
    		Agonist 99.40%
    Polyinosinic-polycytidylic acid (Poly(I:C)) sodium is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid sodium can directly trigger cancer cells to undergo apoptosis.
    Polyinosinic-polycytidylic acid sodium
  • HY-P9930
    Evolocumab
    		Inhibitor 98.40%
    Evolocumab (AMG 145) is a human monoclonal antibody that inhibits PCSK9. Evolocumab is used in the study of hypercholesterolemia and atherosclerotic cardiovascular disease. Evolocumab binds to circulating PCSK9 protein and inhibits its binding to LDLR. Evolocumab has antioxidant and cytoprotective activities against H2O2-induced oxidative damage to endothelial cells. Evolocumab may also negatively regulate activation of the TLR-4/NF-κB signaling pathway to prevent inflammation.
    Evolocumab
  • HY-B0180A
    Imiquimod hydrochloride
    		Agonist 99.77%
    Imiquimod hydrochloride (R 837 hydrochloride), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod hydrochloride exhibits antiviral and antitumor effects in vivo. Imiquimod hydrochloride can be used for the research of external genital, perianal warts, cancer and COVID-19.
    Imiquimod hydrochloride
  • HY-108471
    CU-CPT22
    		Inhibitor ≥99.0%
    CU-CPT22 is a potent protein complex of toll-like receptor 1 and 2 (TLR1/2) inhibitor, and competes with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1/2 with a Ki of 0.41 µM. CU-CPT22 blocks Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58 µM.
    CU-CPT22
  • HY-146244
    Agatolimod
    		Agonist
    Agatolimod (ODN 2006), a class B ODN (oligodeoxynucleotide), is a TLR9 agonist. Agatolimod is also an optimal CpG sequence for humans. Agatolimod stimulates very strong production of NO2 and IL-6 in HD11 cells. Agatolimod can be used for breast cancer research. Sequence: 5'-tcgtcgttttgtcgttttgtcgtt-3'.
    Agatolimod
  • HY-107575
    TLR4-IN-C34
    		Inhibitor 99.90%
    TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis.
    TLR4-IN-C34
  • HY-149652
    IRF5-IN-1
    		Inhibitor 99.91%
    IRF5-IN-1 (compound C5) is an IRF5 pathway-specific inhibitor. IRF5-IN-1 significantly reduces IRF5 nuclear translocation without affecting the activation of NF-κB p65. IRF5-IN-1 acts through SLC15A4 to selectively inhibit TLR7/8-induced IRF5 responses in cells.
    IRF5-IN-1
  • HY-109104
    Telratolimod
    		Agonist 98.98%
    Telratolimod (MEDI9197) is a potent toll like receptors 7/8 (TLR7/8) agonist, with antitumor activity.
    Telratolimod
  • HY-13773
    Motolimod
    		Agonist 98.12%
    Motolimod (VTX-2337;VTX-378) is a selective Toll-like receptor 8 (TLR8) agonist, with an EC50 of approximately 100 nM.
    Motolimod
  • HY-131166
    Curdlan
    		Activator ≥98.0%
    Curdlan is a polysaccharide found in bacteria, consisting of a glucose homopolymer with β-1,3-glycosidic linkages. Curdlan can be recognized by Dectin-1 (a C-type lectin receptor), inducing immune responses in tissue mast cells and enhancing dendritic cell effects in tumor immunity. Curdlan holds potential for research in cancer and immune-inflammatory diseases.
    Curdlan
  • HY-139567
    Afimetoran
    		Antagonist 99.37%
    Afimetoran (BMS-986256) is an orally active, selective, and highly bioavailable TLR7/8 antagonist. Afimetoran (BMS-986256) can inhibit TLR7/8 activation of the NF-κB pathway and reverse TLR7 mediated resistance to steroid induced apoptosis in plasma cell like dendritic cells (pDCs). Afimetoran (BMS-986256) can be used for research on inflammation and autoimmune diseases (systemic lupus erythematosus).
    Afimetoran
  • HY-W021879
    DSRM-3716
    		Inhibitor 99.91%
    DSRM-3716 (5-Iodoisoquinoline) is a potent and selective SARM1 NADase inhibitor with an IC50 of 75 nM. DSRM-3716 is selective against other NAD+-processing enzymes, receptors, and transporters. DSRM-3716 provides robust axon protection.
    DSRM-3716
  • HY-W250113
    Zymosan A
    		Agonist
    Zymosan A (Zymosan A from Saccharomyces cerevisiae) is a TLR2 agonist, that targeting TLRs can prevent and suppress IR-induced intestinal injury. Zymosan A exhibits a significant radioprotective effect, and protects IR-induced intestinal injury in mice. Zymosan A promotes the regeneration of intestinal stem cells (ISCs), after IR injury.
    Zymosan A
  • HY-141537
    ABR-238901
    		Inhibitor 98.71%
    ABR-238901 is an orally active and potent S100A8/A9 blocker and inhibits S100A8/A9 interaction with its receptors RAGE (receptor for advanced glycation endproducts) and TLR4 (toll-like receptor 4). ABR-238901 has the potential for myocardial infarction (MI) research.
    ABR-238901
  • HY-N0680
    Thiamine hydrochloride
    		Inhibitor 99.97%
    Thiamine hydrochloride (Thiamine chloride hydrochloride) is an essential micronutrient needed as a cofactor for many central metabolic enzymes.Thiamine hydrochloride activates NrF-2/HO-1 and inhibits TLR4, NF-κB. Thiamine hydrochloride has neuroprotective and anti-inflammatory effects. Thiamine hydrochloride can be used in the studys of diabetic complications, neurological diseases, cancers, and colitis.
    Thiamine hydrochloride
  • HY-N0462
    Corilagin
    		99.96%
    Corilagin, a gallotannin, has anti-tumor, anti-inflammatory and hepatoprotective activities. Corilagin inhibits activity of reverse transcriptase of RNA tumor viruses. Corilagin also inhibits the growth of Staphylococcus aureus with a MIC of 25 μg/mL. Corilagin shows anti-tumor activity on hepatocellular carcinoma and ovarian cancer model. Corilagin shows low toxicity to normal cells and tissues.
    Corilagin
  • HY-N0201
    Atractylenolide I
    		Antagonist 99.94%
    Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.
    Atractylenolide I
  • HY-150741C
    ODN 2216 sodium
    		Activator
    ODN 2216 sodium is a human-specific TLR9 (toll-like receptor 9) ligand or agonist. ODN 2216 sodium induces high amounts of IFN-α and IFN-β. ODN 2216 sodium induces IFN-α by pDC (plasmacytoid DC) and IL-12 (p40) production by DC (dendritic cells). ODN 2216 sodium stimulates IFN-γ production in peripheral blood mononuclear cells (PBMC), which is indirect and mediated by IFN-α/β. ODN 2216 sodium can activate NK cells and promote IFN-γ production of TCR-triggered CD4+ T cells.
    ODN 2216 sodium
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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